Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C18H21NO4.ClH |
Molecular Weight | 351.825 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@@]12OC3=C4C(C[C@@]5([H])N(C)CC[C@@]14[C@@]5(O)CCC2=O)=CC=C3OC
InChI
InChIKey=MUZQPDBAOYKNLO-RKXJKUSZSA-N
InChI=1S/C18H21NO4.ClH/c1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10;/h3-4,13,16,21H,5-9H2,1-2H3;1H/t13-,16+,17+,18-;/m1./s1
Molecular Formula | C18H21NO4 |
Molecular Weight | 315.3636 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
http://reference.medscape.com/drug/oxycontin-xtampza-er-oxycodone-343321 | https://www.ncbi.nlm.nih.gov/pubmed/23880538 | https://www.drugs.com/oxycodone.html
Curator's Comment: description was created based on several sources, including
http://reference.medscape.com/drug/oxycontin-xtampza-er-oxycodone-343321 | https://www.ncbi.nlm.nih.gov/pubmed/23880538 | https://www.drugs.com/oxycodone.html
Oxycodone is a semisynthetic opioid used for the management of acute and chronic pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Oxycodone is a highly selective full agonist of the μ-opioid receptor (MOR), with low affinity for the δ-opioid receptor (DOR) and κ-opioid receptor (KOR). After oxycodone binds to the MOR, a G protein-complex is released, which inhibits the release of neurotransmitters by the cell by reducing the amount of cAMP produced, closing calcium channels, and opening potassium channels. After a dose of conventional (instant-release) oral oxycodone, the onset of action is 10–30 minutes, and peak plasma levels of the drug are attained within roughly 30–60 minutes in contrast, after a dose of OxyContin (an oral controlled-release formulation), peak plasma levels of oxycodone occur in about three hours. The duration of instant-release oxycodone is 3 to 6 hours, although this can be variable depending on the individual. Oxycodone in the blood is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain. Serious side effects of oxycodone include reduced sensitivity to pain (beyond the pain the drug is taken to reduce), euphoria, anxiolysis, feelings of relaxation, and respiratory depression. Common side effects of oxycodone include constipation (23%), nausea (23%), vomiting (12%), somnolence (23%), dizziness (13%), itching (13%), dry mouth (6%), and sweating (5%).
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL233 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
500.0 nM [EC50] | ||
Target ID: CHEMBL237 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
16000.0 nM [EC50] | ||
Target ID: CHEMBL236 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538 |
4000.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PERCODAN-DEMI Approved UseOxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin is NOT intended for use as a prn analgesic. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as outlined by the World Health Organization, the Agency for Healthcare Research and Quality (formerly known as the Agency for HealthCare Policy and Research), the Federation of State Medical Boards Model Guidelines, or the American Pain Society. OxyContin is not indicated for pain in the immediate postoperative period (the first 12-24 hours following surgery), or if the pain is mild, or not expected to persist for an extended period of time. OxyContin is only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines.) Launch Date1950 |
|||
Primary | PERCODAN-DEMI Approved UseOxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin is NOT intended for use as a prn analgesic. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as outlined by the World Health Organization, the Agency for Healthcare Research and Quality (formerly known as the Agency for HealthCare Policy and Research), the Federation of State Medical Boards Model Guidelines, or the American Pain Society. OxyContin is not indicated for pain in the immediate postoperative period (the first 12-24 hours following surgery), or if the pain is mild, or not expected to persist for an extended period of time. OxyContin is only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines.) Launch Date1950 |
|||
Primary | PERCODAN-DEMI Approved UseOxyContin Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin is NOT intended for use as a prn analgesic. Physicians should individualize treatment in every case, initiating therapy at the appropriate point along a progression from non-opioid analgesics, such as non-steroidal anti-inflammatory drugs and acetaminophen to opioids in a plan of pain management such as outlined by the World Health Organization, the Agency for Healthcare Research and Quality (formerly known as the Agency for HealthCare Policy and Research), the Federation of State Medical Boards Model Guidelines, or the American Pain Society. OxyContin is not indicated for pain in the immediate postoperative period (the first 12-24 hours following surgery), or if the pain is mild, or not expected to persist for an extended period of time. OxyContin is only indicated for postoperative use if the patient is already receiving the drug prior to surgery or if the postoperative pain is expected to be moderate to severe and persist for an extended period of time. Physicians should individualize treatment, moving from parenteral to oral analgesics as appropriate. (See American Pain Society guidelines.) Launch Date1950 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
19 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
|
22.2 ng/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17.7 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
39.3 ng/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
15.7 ng/mL |
5 mg 4 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
12.9 ng/mL |
3.33 mg 6 times / day steady-state, oral dose: 3.33 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
105 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
|
128.2 ng × h/mL |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
133 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
268.2 ng × h/mL |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
113.3 ng × h/mL |
5 mg 4 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
99 ng × h/mL |
3.33 mg 6 times / day steady-state, oral dose: 3.33 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.9 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
|
3.55 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3.3 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
3.85 h |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
55% |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
|
55% |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
55% |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
55% |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
55% |
5 mg 4 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
55% |
3.33 mg 6 times / day steady-state, oral dose: 3.33 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
OXYCODONE unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
30 mg 1 times / day single, oral Studied dose Dose: 30 mg, 1 times / day Route: oral Route: single Dose: 30 mg, 1 times / day Co-administed with:: acetaminophen(1950 mg; single) Sources: cocaine(1/4 g; single) |
healthy, 30 years n = 1 Health Status: healthy Age Group: 30 years Sex: M Population Size: 1 Sources: |
Other AEs: Pulmonary edema... |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 120 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 120 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (grade 1-2, 1.7%) Sources: Page: /nda/98/20932_medr_P2.pdf - p.21Dizziness (grade 1-2, 1.7%) Abdominal pain (grade 1-2, 0.8%) |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 125 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 125 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Disc. AE: Headache, Vomiting... AEs leading to discontinuation/dose reduction: Headache (grade 1-2, 0.8%) Sources: Page: /nda/98/20932_medr_P2.pdf - p.21Vomiting (grade 1-2, 0.8%) Nausea (grade 1-2, 0.8%) Somnolence (grade 1-2, 0.8%) |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 63 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 63 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (grade 1-2, 6.3%) Sources: Page: /nda/98/20932_medr_P2.pdf - p.21Dizziness (grade 1-2, 4.8%) Confusion (grade 1-2, 3.2%) |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 126 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 126 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Disc. AE: Vomiting, Flu syndrome... AEs leading to discontinuation/dose reduction: Vomiting (grade 1-2, 0.8%) Sources: Page: /nda/98/20932_medr_P2.pdf - p.21Flu syndrome (grade 1-2, 0.8%) Confusion (grade 1-2, 0.8%) Fatigue (grade 1-2, 0.8%) |
6 mg 2 times / day single, oral (mean) Studied dose Dose: 6 mg, 2 times / day Route: oral Route: single Dose: 6 mg, 2 times / day Sources: |
healthy, mean age 33 years n = 35 Health Status: healthy Age Group: mean age 33 years Sex: M+F Population Size: 35 Sources: |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (11.4%) Sources: |
15 mg 1 times / day single, oral Studied dose Dose: 15 mg, 1 times / day Route: oral Route: single Dose: 15 mg, 1 times / day Sources: Page: nda/2011/202080Orig1s000MedR.pdf - p.22 |
healthy, mean age 36 years n = 40 Health Status: healthy Age Group: mean age 36 years Sex: M+F Population Size: 40 Sources: Page: nda/2011/202080Orig1s000MedR.pdf - p.22 |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (2.5%) Sources: Page: nda/2011/202080Orig1s000MedR.pdf - p.22 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Pulmonary edema | 30 mg 1 times / day single, oral Studied dose Dose: 30 mg, 1 times / day Route: oral Route: single Dose: 30 mg, 1 times / day Co-administed with:: acetaminophen(1950 mg; single) Sources: cocaine(1/4 g; single) |
healthy, 30 years n = 1 Health Status: healthy Age Group: 30 years Sex: M Population Size: 1 Sources: |
|
Abdominal pain | grade 1-2, 0.8% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 120 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 120 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Dizziness | grade 1-2, 1.7% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 120 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 120 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Nausea | grade 1-2, 1.7% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 120 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 120 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Headache | grade 1-2, 0.8% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 125 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 125 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Nausea | grade 1-2, 0.8% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 125 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 125 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Somnolence | grade 1-2, 0.8% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 125 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 125 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Vomiting | grade 1-2, 0.8% Disc. AE |
20 mg 2 times / day multiple, oral (mean) Recommended Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 125 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 125 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Confusion | grade 1-2, 3.2% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 63 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 63 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Dizziness | grade 1-2, 4.8% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 63 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 63 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Nausea | grade 1-2, 6.3% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 63 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 63 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Confusion | grade 1-2, 0.8% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 126 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 126 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Fatigue | grade 1-2, 0.8% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 126 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 126 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Flu syndrome | grade 1-2, 0.8% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 126 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 126 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Vomiting | grade 1-2, 0.8% Disc. AE |
5 mg 4 times / day multiple, oral Recommended Dose: 5 mg, 4 times / day Route: oral Route: multiple Dose: 5 mg, 4 times / day Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
unhealthy, adult n = 126 Health Status: unhealthy Condition: chronic pain Age Group: adult Sex: M+F Population Size: 126 Sources: Page: /nda/98/20932_medr_P2.pdf - p.21 |
Vomiting | 11.4% Disc. AE |
6 mg 2 times / day single, oral (mean) Studied dose Dose: 6 mg, 2 times / day Route: oral Route: single Dose: 6 mg, 2 times / day Sources: |
healthy, mean age 33 years n = 35 Health Status: healthy Age Group: mean age 33 years Sex: M+F Population Size: 35 Sources: |
Vomiting | 2.5% Disc. AE |
15 mg 1 times / day single, oral Studied dose Dose: 15 mg, 1 times / day Route: oral Route: single Dose: 15 mg, 1 times / day Sources: Page: nda/2011/202080Orig1s000MedR.pdf - p.22 |
healthy, mean age 36 years n = 40 Health Status: healthy Age Group: mean age 36 years Sex: M+F Population Size: 40 Sources: Page: nda/2011/202080Orig1s000MedR.pdf - p.22 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | ||||
minor | ||||
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: When both oxidative pathways of the metabolism of oxycodone were inhibited with paroxetine and itraconazole (CYP3A4 AND CYP2D6 inhibitors), the mean AUC(0,∞) of oxycodone increased by 2.9-fold (P < 0.001), and its Cmax by 1.8-fold (P < 0.001). Page: 7.0 |
|||
yes | yes (co-administration study) Comment: When both oxidative pathways of the metabolism of oxycodone were inhibited with paroxetine and itraconazole (CYP3A4 AND CYP2D6 inhibitors), the mean AUC(0,∞) of oxycodone increased by 2.9-fold (P < 0.001), and its Cmax by 1.8-fold (P < 0.001). |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Advancement of opioid analgesia with controlled-release oxycodone. | 2001 |
|
"No, Duke. No divorce". | 2001 Aug 20 |
|
A curse and a cure. Is the crackdown on an abused drug causing needless suffering? | 2001 Aug 6 |
|
Opioid analgesic prescribing and use - an audit of analgesic prescribing by general practitioners and The Multidisciplinary Pain Centre at Royal Brisbane Hospital. | 2001 Dec |
|
Addressing OxyContin abuse. | 2001 Jul-Aug |
|
I.v. ketoprofen for analgesia after tonsillectomy: comparison of pre- and post-operative administration. | 2001 Mar |
|
Narcotic analgesics for dental pain: available products, strengths, and formulations. | 2001 Mar-Apr |
|
Drug dependence studies and regulations: an overview of the past and present. | 2001 Nov |
|
The use of oxycodone in cancer-related pain: a literature review. | 2001 Nov |
|
Acetaminophen, aspirin, or Ibuprofen in combination analgesic products. | 2001 Nov-Dec |
|
Managing postoperative pain. | 2001 Sep |
|
Interscalene brachial plexus block with continuous intraarticular infusion of ropivacaine. | 2001 Sep |
|
Oxycodone and oxycontin. | 2001 Sep 17 |
|
Valdecoxib. | 2002 |
|
Oxycodone/ibuprofen. | 2002 |
|
The simultaneous determination of codeine, morphine, hydrocodone, hydromorphone, 6-acetylmorphine, and oxycodone in hair and oral fluid. | 2002 Apr |
|
Capillary electrophoresis and capillary electrophoresis-ion trap multiple-stage mass spectrometry for the differentiation and identification of oxycodone and its major metabolites in human urine. | 2002 Apr 25 |
|
More blame and praise for a pain drug. | 2002 Apr 29 |
|
Severe chronic renal failure in association with oxycodone addiction: a new form of fibrillary glomerulopathy. | 2002 Aug |
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Minimal interaction between gatifloxacin and oxycodone. | 2002 Aug |
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Nasal administration of opioids for pain management in adults. | 2002 Aug |
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Treatment of postherpetic neuralgia: a systematic review of the literature. | 2002 Feb |
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Comparison of pre- and postoperative administration of ketoprofen for analgesia after tonsillectomy in children. | 2002 Feb |
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Treatment of painful sickle cell leg ulcers with topical opioids. | 2002 Feb 1 |
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Recovery after tonsillectomy in adults: a three-week follow-up study. | 2002 Jan |
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A comparison of oral transmucosal fentanyl citrate and oral oxycodone for pediatric outpatient wound care. | 2002 Jan-Feb |
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Perioperative management in children with sickle cell disease undergoing laparoscopic surgery. | 2002 Jan-Mar |
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Safety and efficacy of controlled-release oxycodone: a systematic literature review. | 2002 Jul |
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Gateways to clinical trials. | 2002 Jul-Aug |
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OxyContin and neonatal abstinence syndrome. | 2002 Jun |
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An evaluation of the efficacy and tolerability of oral tramadol hydrochloride tablets for the treatment of postsurgical pain in children. | 2002 Jun |
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Comparison of the opioid-sparing efficacy of diclofenac and ketoprofen for 3 days after knee arthroplasty. | 2002 Mar |
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Validity and reliability of three commercially available breath-by-breath respiratory systems. | 2002 Mar |
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[Chronic pain of the musculoskeletal system. Make your patients move!]. | 2002 Mar 14 |
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Pain management after major orthopaedic surgery: current strategies and new concepts. | 2002 Mar-Apr |
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From physician to inmate. | 2002 May |
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The analgesic efficacy of valdecoxib vs. oxycodone/acetaminophen after oral surgery. | 2002 May |
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Oral ondansetron, tropisetron or metoclopramide to prevent postoperative nausea and vomiting: a comparison in high-risk patients undergoing thyroid or parathyroid surgery. | 2002 May |
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Sevoflurane versus halothane: effect of oxycodone premedication on emergence behaviour in children. | 2002 May |
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A randomized controlled trial of early oral analgesia in gynecologic oncology patients undergoing intra-abdominal surgery. | 2002 May |
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Simultaneous quantitation of opioids in blood by GC-EI-MS analysis following deproteination, detautomerization of keto analytes, solid-phase extraction, and trimethylsilyl derivatization. | 2002 Oct |
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Detection of cocaine analytes and opiates in nails from postmortem cases. | 2002 Oct |
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Pharmacogenomics as molecular autopsy for postmortem forensic toxicology: genotyping cytochrome P450 2D6 for oxycodone cases. | 2002 Oct |
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Determination of 6-oxo-morphinans, as the oximes, by difference circular dichroism spectroscopy. | 2002 Oct |
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Propacetamol as adjunctive treatment for postoperative pain after cardiac surgery. | 2002 Oct |
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Massive OxyContin ingestion refractory to naloxone therapy. | 2002 Oct |
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Induced hypothermia for drug overdose. | 2002 Sep |
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Interscalene brachial plexus block is superior to subacromial bursa block after arthroscopic shoulder surgery. | 2002 Sep |
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Review: tricyclic antidepressants, capsaicin, gabapentin, and oxycodone are effective for postherpetic neuralgia. | 2002 Sep-Oct |
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Oxycontin--misuse and abuse. | 2002 Summer |
Sample Use Guides
For opioid naïve patients, initiate treatment with 5 mg to 15 mg every 4 to 6 hours as needed for pain.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23880538
Human embryonic kidney (HEK)-293 were used for activity evaluation. Receptor G protein-mediated responses were determined by measuring changes in cAMP using the cAMP–homogenous timeresolved fluorescence kit (Cisbio, Codolet, France). MOR, KOR, DOR all couple to Gai so G protein coupling was measured as inhibition of forskolin-stimulated cAMP accumulation in the presence of 1.5 mkM NKH-477 (water-soluble forskolin, Tocris catalog #1603) and 500 mkM 3-isobutyl-1-methylxanthine (IBMX). cAMP accumulation assays were run in parallel with b-arrestin-2 recruitment, using the same cells, drug dilutions, and assay buffers [1% dimethylsulfoxide (DMSO), F12 Ham’s buffer] to ensure accurate assay-to-assay comparisons of data. Plates were read using a time-resolved fluorescence ratio (665 nm/620 nm) on a PheraStar plate reader
Substance Class |
Chemical
Created
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on
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Fri Dec 15 15:04:36 GMT 2023
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on
Fri Dec 15 15:04:36 GMT 2023
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Record UNII |
C1ENJ2TE6C
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Validated (UNII)
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DEA NO. |
9143
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NCI_THESAURUS |
C67413
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NCI_THESAURUS |
C1506
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7859
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C48010
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124-90-3
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C1ENJ2TE6C
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5462350
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82063
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1485205
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SUB03583MIG
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DTXSID80924674
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C1ENJ2TE6C
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204-717-1
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100000090368
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m8328
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CHEMBL656
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DBSALT000277
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Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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||
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PARENT -> SALT/SOLVATE | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
sum of impurities D and E: not more than 10 times the area of the peak due to oxycodone in the chromatogram obtained with reference solution (b) (1.0 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
sum of impurities D and E: not more than 10 times the area of the peak due to oxycodone in the chromatogram obtained with reference solution (b) (1.0 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
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ACTIVE MOIETY |